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Potency with potential: 2-Phenoxy-nicotinamides were identified as potent agonists at the GPBAR1 receptor, a target in the treatment of obesity, type 2 diabetes and metabolic syndrome. Extensive… (More)
SAR studies of a recently described SST5R selective benzoxazole piperidine lead series are described with particular focus on the substitution pattern on the benzyl and benzoxazole side-chains.… (More)
Pyrimidine alkynes can be transformed into the corresponding annulated pyridines efficiently in flow. The superheating of organic solvents far beyond their boiling point enables toxic and difficult… (More)
Abstract Treatment of [1,3,5]triazine-2,4,6-tricarboxylic acid triethyl ester ( 4 ) with arylhydrazines provided 5-amino-6-oxo-1,6-dihydro[1,2,4]triazine-3-carboxylic acid ethyl esters 5a – g in… (More)
The reaction of various pyrimidine alkynes proceeds with the expulsion of cyanides and provides facile access to the novel annulated pyridine building blocks.
Macrocyclic inhibitors of rhodesain (RD), a parasitic cysteine protease and drug target for the treatment of human African trypanosomiasis, have shown low metabolic stability at the macrocyclic ether… (More)